Acetylcholine neurotransmitter and its influence on the body and brain - Function of this brain chemical and how to raise levels
How to Increase acetylcholine naturally with supplements and herbs
April 24 2018 by Ray Sahelian, M.D.

Acetylcholine was the very first neurotransmitter to be identified back in the early 1900s. It is made simply from choline and a two-carbon molecule called acetyl. Dietary choline and phosphatidylcholine (also known as lecithin) serve as the sources of free choline for acetylcholine synthesis. This neurotransmitter is present in the brain and the peripheral nervous system, and acetylcholine receptors are found widely throughout the body and brain. In the brain, acetylcholine is involved in learning and memory. It also stimulates muscle tissue. Acetylcholine is involved in Alzheimer's disease.

How to Increase acetylcholine levels in a natural way
Supplements such as  bitartrate and CDP-choline raise levels of acetylcholine. They are both available without a prescription. Acetylcholine, itself, is not available in supplement pill form. Ginseng and ginkgo biloba may be other herbal alternatives and there are probably other supplements that have an influence that we will find out over time.

Choline is an essential precursor of acetylcholine. It also helps in the production of lipotropic agents which converts fats into useful products and aids in the production of HDL (good) cholesterol. 100 % natural choline bound to tartaric acid, making it easier to absorb.

 

DMAE, Pantothenic acid, Inositol, Trimethylglycine, Methylcobalamin, Tyrosine, and vinpocetine.

Effect of combination of extracts of ginseng and ginkgo biloba on acetylcholine in amyloid beta-protein-treated rats.
Acta Pharmacologica Sinica. 2004.
To determine the concentration of acetylcholine in amyloid beta-protein treated rats and offer a method determining acetylcholine as well. A 1-month combination of extracts of ginseng and ginkgo biloba (Naoweikang) administration to rats was performed daily after bilateral injection of amyloid beta-protein for each side into hippocampus. Naoweikang significantly increased the level of acetylcholine in whole brain of amyloid beta-protein treated rats.

Q. Can you please let me know how to best ways to raise acetylcholine levels in the brain? I am specifically interested in rising levels in the area of the brain which controls cognitive function. Also, for example, if dopamine has been suppressed due to the use of anti-psychotics for many years, such as Prolixin, would now raising the acetylcholine levels be able to improve cognitive function?
    A. Rather than focusing on one or two neurotransmitters, it is better to try to enhance several aspects of brain function. Using supplements such as choline or cdp-choline can raise acetylcholine levels. It is difficult to predict in any one individual which supplement or combination formula would work best.


Acetylcholine blocking drugs and cognitive decline
Elderly people who take commonly prescribed drugs for incontinence, allergy or high blood pressure are less able to take care of themselves, function worse than others in the same age group who don't take these drugs, and walk slower. Drugs that block acetylcholine, which is important for memory, hasten cognitive decline in elderly people.

Sexuality and erections, erectile function
Acetylcholine is a neurotransmitter that helps facilitate erectile function. Thus, choline supplements could help some men achieve better erections. See Passion Rx for a highly effective libido support product formulated by Dr. Sahelian for men and women.

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Chemistry and function, how does it work?
Once produced, acetylcholine is stored in brain cells and released into the synaptic cleft upon stimulation. When released into the synaptic cleft, the enzyme acetylcholinesterase breaks acetylcholine back down into choline and acetyl. In Alzheimer’s disease, there is a shortage of acetylcholine, and one of the ways doctors have tried to increase the levels of this neurotransmitter is by prescribing drugs, such as tacrine and galantamine, that inhibit the enzyme acetylcholinesterase. An alternative to these drugs, a Chinese herbal extract called huperzine A, can also inhibit this enzyme. Galantamine is now available without a prescription.

Appetite influence
The description of acetylcholine neurotransmitter clearly states how it has been shown to improve brain function and sex drive, nothing about appetite reduction was included. Are you aware of any?
    It probably has some mild appetite suppressing activity.

Blood vessel dilation
Acetylcholine -induced vasodilation is mediated by nitric oxide and prostaglandins in human skin.
J Appl Physiol. 2005.
Acetylcholine can effect vasodilation by several mechanisms, including activation of endothelial nitric oxide synthase and prostaglandin production.

Ghrelin influence
Acetylcholine regulates ghrelin secretion in humans.
J Clin Endocrinol Metabolism. 2004.
Ghrelin secretion has been reportedly increased by fasting and energy restriction but decreased by food intake, glucose, insulin, and somatostatin. However, its regulation is still far from clarified. The cholinergic system (with acetylcholine) mediates some ghrelin actions, e.g. stimulation of gastric contractility and acid secretion and its orexigenic activity. To clarify whether ghrelin secretion undergoes cholinergic control in humans, we studied the effects of pirenzepine (PZ), a muscarinic antagonist, or pyridostigmine (PD), an indirect cholinergic agonist, on ghrelin, GH, insulin, and glucose levels in six normal subjects. We find that ghrelin secretion is under cholinergic, namely muscarinic, control in humans.

Sleep and memory
Low acetylcholine during slow-wave sleep is critical for declarative memory consolidation.
University of Lubeck, Ratzeburger Allee Lubeck, Germany. Proc Natl Acad Sci U S A. 2004.
The neurotransmitter acetylcholine is considered essential for proper functioning of the hippocampus-dependent declarative memory system, and it represents a major neuropharmacological target for the treatment of memory deficits, such as those in Alzheimer's disease. During slow-wave sleep, however, declarative memory consolidation is particularly strong, while acetylcholine levels in the hippocampus drop to a minimum. Our findings are in line with predictions that a low cholinergic tone during slow wave sleep is essential for declarative memory consolidation.

Vision
Effects of cholinergic enhancement on visual stimulation, spatial attention, and spatial working memory.
Neuron. 2004.
We compared behavioral and neural effects of cholinergic enhancement between spatial attention, spatial working memory, and visual control tasks, using fMRI and the anticholinesterase physostigmine. Physostigmine speeded responses nonselectively but increased accuracy selectively for attention. Physostigmine also decreased activations to visual stimulation across all tasks within primary visual cortex, increased extrastriate occipital cortex activation selectively during maintained attention and WM encoding, and decreased parietal activation selectively during maintained attention. While cholinergic enhancement facilitates visual attention by increasing activity in extrastriate cortex generally, it accomplishes this in a manner that reduces expectation-driven selective biasing of extrastriate cortex.

Side effects, safety
If you have hyperhidrosis, a condition known as excessive sweating, you may with to avoid nutrients that increase acetylcholine levels such as choline.

Drugs and medications that interfere
Medicines taken by millions for depression, asthma, allergies, and other conditions may raise that risk for dementia. The drugs are known as anticholinergics. They work by blocking the brain chemical called acetylcholine, which is crucial for memory. Many over-the-counter and prescription drugs work in this way, ranging from the antidepressant Paxil (paroxetine) to the allergy drug Benadryl (diphenhydramine) to the motion sickness remedy Dramamine (dimenhydrinate).

Acetylcholine Research study
Cytidine and Uridine Increase Striatal CDP-Choline Levels Without Decreasing Acetylcholine Synthesis or Release.
Cell Mol Neurobiology. 2006; Ulus IH, Watkins CJ, Wurtman RJ. Department of Pharmacology and Clinical Pharmacology, Uludag University Medical School, Bursa, Turkey.
Treatments that increase acetylcholine release from brain slices decrease the synthesis of phosphatidylcholine by, and its levels in, the slices. Our data show that cytidine and uridine can stimulate brain phosphatide synthesis without diminishing acetylcholine synthesis or release.

Questions
Q. I produce too much acetylcholine and the acetylcholinesterase in my system is very low. Because my acetylcholinesterase is not working properly, I give off a fish odour. Can you recommend a supplement to increase the acetylcholinesterase enzyme?
   A. I don't know.

Q. I have a cholinesterase deficiency and cannot take succinylcholine type drug. It is heritary in my family. I was tested and my levels were like the worse. I have no cholineasterase to break down acetylcholine causing sever muscle contractions that last forever. Will I benefit from CDP Choline.
   A. As of 2018 I do not know the answer.

I recently read your article on acetylcholine. I'm particularly interested in the section that included, "Acetylcholine blocking drugs and cognitive decline" I had unfortunately fallen down a road of abusing diphenhydramine. Over the course of a year I had worked up from 25 mg to about 450 mg a day. I have been off it now for about a month and can feel my cognitive function are beginning to rebound. I'm 35 yo male and 200 lb. As I did research I ran into the fact that diphenhydramine blocks Acetylcholine, like little pink Alzheimer's in a bottle. So I'm looking for supplements that may help my system rejuvenate its choline process. I have NOT taken any supplements yet. But I did get a choline blend supplement with 150 mg citicoline (CDP Choline) and 150mg Alpha GPC per 1 day serving. I'm not sure if this might be a good direction to start. Or is there any additional or alternative suggestions i.e. Galatamine or Huperzine? I also read about the receptors such as the Nicotinic Acetylcholine receptors. Could those receptors be impaired or diminished? Are there any supplements that could aid them? And I do know first and foremost the importance of receiving help for addiction, in which I have. Basically what would be a good course to research with supplements that may aid me in restoring the choline process in my brain/body?
   A. It is worthwhile trying the supplements you have purchased, others to try include carnosine and acetylcarnitine.